Sunday 
 
 
2:00 pm - 9:00 pm 
	
Arrival and Check-in
 
 
						
6:00 pm - 7:00 pm 
	
Dinner
 
 
						
7:30 pm - 7:40 pm 
	
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
 
 
						
7:40 pm - 9:30 pm 
	
Small Molecule Approaches for Immuno-Oncology 
 
 
 
						
7:40 pm - 8:10 pm 
	
"A Medicinal Chemist’s Primer to Immuno-Oncology: Case Study on the Development of Small Molecule CXCR4 Antagonists" 
 
 
 
						
8:10 pm - 8:15 pm 
	
Discussion
 
 
						
8:15 pm - 8:45 pm 
	
"Phenotypic Discovery and Optimization of Potent T-Cell Modulators: Dual Inhibition of Diacylglycerol Kinases Alpha and Zeta" 
 
 
 
						
8:45 pm - 8:50 pm 
	
Discussion
 
 
						
8:50 pm - 9:20 pm 
	
"Discovery of HTL0039732: A Potent and Selective EP4 Receptor Antagonist for Cancer Immunotherapy" 
 
 
 
						
9:20 pm - 9:30 pm 
	
Discussion
 
 
						
	Monday 
 
 
7:30 am - 8:30 am 
	
Breakfast
 
 
						
9:00 am - 12:30 pm 
	
Emerging Technologies: From In Silico to Implementation 
 
 
 
						
9:00 am - 9:30 am 
	
"AI-Driven Drug Discovery Delivers A2AR Antagonist Clinical Candidate" 
 
 
 
						
9:30 am - 9:45 am 
	
Discussion
 
 
						
9:45 am - 10:15 am 
	
"Case Studies Utilizing an In Silico ADMET Toolbox to Prioritize Chemical Series with a High Probability of Success" 
 
 
 
						
10:15 am - 10:30 am 
	
Discussion
 
 
						
10:30 am - 11:00 am 
	
Coffee Break
 
 
						
11:00 am - 11:30 am 
	
"In Silico Driven Drug Discovery of a Zwitterionic Integrin αvβ6 Development Candidate for Fibrosis" 
 
 
 
						
11:30 am - 11:45 am 
	
Discussion
 
 
						
11:45 am - 12:15 pm 
	
"Motion-Based Drug Designâ„¢ in Action: Discovery of RLY-4008, an Isoform Selective, Irreversible Small Molecule Inhibitor of FGFR2" 
 
 
 
						
12:15 pm - 12:30 pm 
	
Discussion
 
 
						
12:30 pm - 1:30 pm 
	
Lunch
 
 
						
1:30 pm - 4:00 pm 
	
Free Time
 
 
						
4:00 pm - 6:00 pm 
	
Poster Session 
 
 
						
6:00 pm - 7:00 pm 
	
Dinner
 
 
						
7:30 pm - 9:30 pm 
	
Therapies Targeting Diseases of the CNS 
 
 
 
						
7:30 pm - 8:00 pm 
	
"Discovery of MK-1468: An Exquisitely Selective, CNS Penetrant LRRK2 Inhibitor for the Treatment of Parkinson’s Disease" 
 
 
 
						
8:00 pm - 8:10 pm 
	
Discussion
 
 
						
8:10 pm - 8:40 pm 
	
"The Discovery and First Disclosure of MIJ821, a Novel, Rapidly Acting Antidepressant" 
 
 
 
						
8:40 pm - 8:50 pm 
	
Discussion
 
 
						
8:50 pm - 9:20 pm 
	
"Discovery of a Clinical Stage OGA Inhibitor and Companion PET tracer for the Treatment of Alzheimer’s Disease" 
 
 
 
						
9:20 pm - 9:30 pm 
	
Discussion
 
 
						
	Tuesday 
 
 
7:30 am - 8:30 am 
	
Breakfast
 
 
						
9:00 am - 12:30 pm 
	
Synthetic Technologies to Enable Medicinal Chemistry 
 
 
 
						
9:00 am - 9:30 am 
	
"How Flow Chemistry Can Impact Drug Discovery: An Automated Tool to Access Novel Chemical Space with Improved Fsp3" 
 
 
 
						
9:30 am - 9:45 am 
	
Discussion
 
 
						
9:45 am - 10:15 am 
	
"Emerging Synthetic Technologies in Fragment-Based Drug Discovery" 
 
 
 
						
10:15 am - 10:30 am 
	
Discussion
 
 
						
10:30 am - 11:00 am 
	
Group Photo / Coffee Break
 
 
						
11:00 am - 11:30 am 
	
"Selective Catalytic Isomerization Reactions" 
 
 
 
						
11:30 am - 11:45 am 
	
Discussion
 
 
						
11:45 am - 12:15 pm 
	
"Genetic Nanomedicine: State of the Art, Frontiers, and Current Research" 
 
 
 
						
12:15 pm - 12:30 pm 
	
Discussion
 
 
						
12:30 pm - 1:30 pm 
	
Lunch
 
 
						
1:30 pm - 4:00 pm 
	
Free Time
 
 
						
4:00 pm - 6:00 pm 
	
Poster Session 
 
 
						
6:00 pm - 7:00 pm 
	
Dinner
 
 
						
7:30 pm - 9:30 pm 
	
Recent Advances in Protein Degraders 
 
 
 
						
7:30 pm - 8:00 pm 
	
"Family-centric Screening Enables the Development of Selective HDAC Degraders" 
 
 
 
						
8:00 pm - 8:10 pm 
	
Discussion
 
 
						
8:10 pm - 8:40 pm 
	
"Discovery of CFT7455: A Potent IKZF1/3 Degrader with Enhanced Catalytic and Pharmacological Properties" 
 
 
 
						
8:40 pm - 8:50 pm 
	
Discussion
 
 
						
8:50 pm - 9:20 pm 
	
"Driving the Design of Induced Proximity Modulators via Ternary Structure Ensembles from MD+HDX" 
 
 
 
						
9:20 pm - 9:30 pm 
	
Discussion
 
 
						
	Wednesday 
 
 
7:30 am - 8:30 am 
	
Breakfast
 
 
						
9:00 am - 12:30 pm 
	
Strategies for Overcoming Drug Safety Liabilities 
 
 
 
						
9:00 am - 9:30 am 
	
"Gut-Targeted GPR40 Agonists to Engage the Gut-Brain Axis" 
 
 
 
						
9:30 am - 9:45 am 
	
Discussion
 
 
						
9:45 am - 10:15 am 
	
"Overcoming an Ames-positive Lead to Enable the Discovery of mGluR2 Negative Allosteric Modulator MK-8768" 
 
 
 
						
10:15 am - 10:30 am 
	
Discussion
 
 
						
10:30 am - 11:00 am 
	
Coffee Break
 
 
						
11:00 am - 11:30 am 
	
"Challenges with the Prediction of Fraction Metabolized by CYPs and Application of New Strategies to the Cardiac Myosin Inhibitor Aficamten " 
 
 
 
						
11:30 am - 11:45 am 
	
Discussion
 
 
						
11:45 am - 12:15 pm 
	
"Abx MCP RG6006 - a Tethered Macrocyclic Peptide Targeting Acinetobacter" 
 
 
 
						
12:15 pm - 12:30 pm 
	
Discussion
 
 
						
12:30 pm - 1:30 pm 
	
Lunch
 
 
						
1:30 pm - 4:00 pm 
	
Free Time
 
 
						
4:00 pm - 6:00 pm 
	
Poster Session 
 
 
						
6:00 pm - 7:00 pm 
	
Dinner
 
 
						
7:30 pm - 9:30 pm 
	
New Directions in Beyond 500 Compounds: From PK to the Clinic 
 
 
 
						
7:30 pm - 8:00 pm 
	
"An Adaptable Toolkit for BRo5 Property Engineering Delivers Permeable KRAS-targeting Peptides" 
 
 
 
						
8:00 pm - 8:10 pm 
	
Discussion
 
 
						
8:10 pm - 8:40 pm 
	
"The Discovery and Development of Lenacapavir (GS-6207): a Twice-Yearly Injectable or Orally Dosed First-in-Class HIV Capsid Inhibitor" 
 
 
 
						
8:40 pm - 8:50 pm 
	
Discussion
 
 
						
8:50 pm - 9:20 pm 
	
"Targeted Protein Degrader Pharmacokinetics: Optimizing towards Oral Bioavailability" 
 
 
 
						
9:20 pm - 9:30 pm 
	
Discussion
 
 
						
	Thursday 
 
 
7:30 am - 8:30 am 
	
Breakfast
 
 
						
8:30 am - 9:00 am 
	
Business Meeting 
Nominations for the Next Vice Chair(s); Complete the GRC Evaluation Forms; Discuss Future Dates and Venue; Election of the Next Vice Chair(s) 
 
 
						
9:00 am - 12:30 pm 
	
Late-Breaking Topics: First Disclosures of Clinical Candidates 
 
 
 
						
9:00 am - 9:30 am 
	
"GS-4224: A Potent, Oral Small Molecule PD-L1 Inhibitor" 
 
 
 
						
9:30 am - 9:45 am 
	
Discussion
 
 
						
9:45 am - 10:15 am 
	
"Discovery of NDI-034858, a Highly Potent and Selective TYK2-JH2 Inhibitor for the Treatment of Autoimmune Diseases, through Structure-based Drug Design" 
 
 
 
						
10:15 am - 10:30 am 
	
Discussion
 
 
						
10:30 am - 11:00 am 
	
Coffee Break
 
 
						
11:00 am - 11:30 am 
	
"Discovery of the MC4R Antagonist PF-07258669 as a Potential Treatment for Appetite Loss" 
 
 
 
						
11:30 am - 11:45 am 
	
Discussion
 
 
						
11:45 am - 12:15 pm 
	
"Discovery of DNL343: a Potent Selective and Brain-penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases" 
 
 
 
						
12:15 pm - 12:30 pm 
	
Discussion
 
 
						
12:30 pm - 1:30 pm 
	
Lunch
 
 
						
1:30 pm - 4:00 pm 
	
Free Time
 
 
						
4:00 pm - 6:00 pm 
	
Poster Session 
 
 
						
6:00 pm - 7:00 pm 
	
Dinner
 
 
						
7:30 pm - 9:30 pm 
	
Keynote Session: Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery 
 
 
 
						
7:30 pm - 8:30 pm 
	
"Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery" 
 
 
 
						
8:30 pm - 8:55 pm 
	
Discussion
 
 
						
8:55 pm - 9:15 pm 
	
General Discussion
 
 
						
9:15 pm - 9:30 pm 
	
Closing Remarks
 
 
						
	Friday 
 
 
7:30 am - 8:30 am 
	
Breakfast
 
 
						
9:00 am 
	
Departure